1637254-93-3Relevant articles and documents
Minimalist linkers suitable for irreversible inhibitors in simultaneous proteome profiling, live-cell imaging and drug screening
Guo, Cuiping,Chang, Yu,Wang, Xin,Zhang, Chengqian,Hao, Piliang,Ding, Ke,Li, Zhengqiu
, p. 834 - 837 (2019)
Activity-based protein profiling (ABPP) and bioimaging have been powerful approaches for in situ drug screening and target identification. However, these approaches are still hindered by the preparation of high-quality probes. To address this challenge, we developed a series of novel minimalist linkers for irreversible inhibitors by incorporation of various bioorthogonal handles into an α,β-unsaturated amide, a common moiety of many irreversible inhibitors. The linker-containing probes have been demonstrated to be suitable for simultaneous protein labelling, live cell imaging and drug screening.
4 - (Substituted phenylamino) aminoquin oxazolines, preparation method and application thereof
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, (2018/01/11)
The invention specifically relates to novel 4-(substituted phenylamino)quinazoline compounds with antineoplastic activity and a preparation method thereof, belonging to the field of pharmaceutical chemical engineering. The 4-(substituted phenylamino)quinazoline compounds have an effective irreversible inhibiting effect on tyrosine kinase and/or good in-vivo pharmacokinetic behavior and are an effective tyrosine kinase irreversible inhibitor.
Aminoquinazoline Derivative And Use Thereof In Preparing Anti-Malignant Tumor Medicament
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Paragraph 0031; 0032, (2015/03/16)
The invention discloses a new amino-quinazoline derivative and its use in preparing drugs for preventing and/or treating malignancies. The amino-quinazoline derivative of the invention is an ideal, high effective, dual and irreversible EGFR and HER2 kinas